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Synthesis and biological evaluation of novel thiazolidinedione analogues as 15-hydroxyprostaglandin dehydrogenase inhibitors.

Authors :
Wu Y
Karna S
Choi CH
Tong M
Tai HH
Na DH
Jang CH
Cho H
Source :
Journal of medicinal chemistry [J Med Chem] 2011 Jul 28; Vol. 54 (14), pp. 5260-4. Date of Electronic Publication: 2011 Jun 29.
Publication Year :
2011

Abstract

Novel thiazolidinedione analogues as 15-hydroxyprostaglandin dehydrogenase (15-PGDH) inhibitors were synthesized. Compounds 2, 3, and 4 exhibited IC(50) of 25, 8, and 19 nM, respectively. They also significantly increased levels of PGE(2) in A549 cells. To assess the influence of 15-PGDH inhibitor on cochlear blood flow (CBF), 2 was applied intravenously to guinea pigs. It increased their CBFs. Scratch wounds were also analyzed in confluent monolayers of HaCaT cells. Cells exposed to 4 showed significantly improved wound healing with respect to a control.

Details

Language :
English
ISSN :
1520-4804
Volume :
54
Issue :
14
Database :
MEDLINE
Journal :
Journal of medicinal chemistry
Publication Type :
Academic Journal
Accession number :
21650226
Full Text :
https://doi.org/10.1021/jm200390u